Results 21 to 30 of about 1,835 (190)

Computational Methods for the Discovery and Optimization of TAAR1 and TAAR5 Ligands

International Journal of Molecular Sciences
G-protein-coupled receptors (GPCRs) represent a family of druggable targets when treating several diseases and continue to be a leading part of the drug discovery process.
Cichero, Elena, Stefano Espinoza, Brullo C., Espinoza, Stefano, Espinoza S., Chiara Brullo, Elena Cichero, Scarano N., Naomi Scarano, Cichero E., Scarano, Naomi, Brullo, Chiara   +11 more
core   +5 more sources

Preclinical development of [¹⁸F]TAAR1-2203 as a PET radioligand for imaging TAAR1 expression and receptor occupancy. [PDF]

Eur J Nucl Med Mol Imaging
Abstract Purpose Trace amine-associated receptor 1 (TAAR1) is an emerging therapeutic target with various implications in neuropsychiatric and metabolic disorders. However, the absence of a suitable positron emission tomography (PET) radioligand has precluded non-invasive
Haider A, Xiao Z, Chen J, Pfister SK, Zhou X, Li Y, Chaudhary A, Zhao C, Rong J, Paehler A, Mohr S, Norcross RD, Honer M, Mu L, Gobbi L, Schibli R, Hoener MC, Liang SH.   +17 more
europepmc   +4 more sources

TAAR1 and Psychostimulant Addiction

Cellular and Molecular Neurobiology, 2020
Trace amine-associated receptor 1 is one of the best-characterized receptors of trace amines. Growing evidence shows that TAAR1 negatively regulates the monoaminergic activity, including dopamine transmission in the mesocorticolimbic system. Neurochemical assays demonstrated that selective TAAR1 full and partial agonists were effective to prevent ...
Jianfeng, Liu, Ruyan, Wu, Jun-Xu, Li
openaire   +3 more sources

Trace Amine-Associated Receptor 1 Modulates the Locomotor and Sensitization Effects of Nicotine

Frontiers in Pharmacology, 2018
Trace amine-associated receptor 1 (TAAR1) has emerged as a promising target for addiction treatments because it affects dopamine transmission in the mesolimbic pathway.
Ilya Sukhanov, Ilya Sukhanov, Ilya Sukhanov, Mariia Dorofeikova, Antonina Dolgorukova, Artem Dorotenko, Raul R. Gainetdinov, Raul R. Gainetdinov   +7 more
doaj   +1 more source

Non-Functional Trace Amine-Associated Receptor 1 Variants in Patients With Mental Disorders

Frontiers in Pharmacology, 2019
Background: The G protein–coupled receptor (GPCR) trace amine-associated receptor 1 (TAAR1) is expressed across brain areas involved in emotions, reward and cognition, and modulates monoaminergic and glutamatergic neurotransmissions.
Grazia Rutigliano, Grazia Rutigliano, Julia Bräunig, Claudia Del Grande, Vittoria Carnicelli, Isabella Masci, Sergio Merlino, Gunnar Kleinau, Luca Tessieri, Simone Pardossi, Sarah Paisdzior, Liliana Dell’Osso, Heike Biebermann, Riccardo Zucchi   +13 more
doaj   +1 more source

Genetic Polymorphisms Affect Mouse and Human Trace Amine-Associated Receptor 1 Function.

PLoS ONE, 2016
Methamphetamine (MA) and neurotransmitter precursors and metabolites such as tyramine, octopamine, and β-phenethylamine stimulate the G protein-coupled trace amine-associated receptor 1 (TAAR1).
Xiao Shi, Nicole A R Walter, John H Harkness, Kim A Neve, Robert W Williams, Lu Lu, John K Belknap, Amy J Eshleman, Tamara J Phillips, Aaron Janowsky   +9 more
doaj   +1 more source

Discovery of Guanfacine as a Novel TAAR1 Agonist: A Combination Strategy through Molecular Modeling Studies and Biological Assays

Pharmaceuticals, 2023
Trace amine-associated receptor 1 (TAAR1) is an attractive target for the design of innovative drugs to be applied in diverse pharmacological settings. Due to a non-negligible structural similarity with endogenous ligands, most of the agonists developed ...
Elena Cichero, Valeria Francesconi, Beatrice Casini, Monica Casale, Evgeny Kanov, Andrey S. Gerasimov, Ilya Sukhanov, Artem Savchenko, Stefano Espinoza, Raul R. Gainetdinov, Michele Tonelli   +10 more
doaj   +1 more source

Developing Thyronamine Analog Pharmaceuticals Targeting TAAR1 to Treat Methamphetamine Addiction [PDF]

, 2013
As a part of the overall program in the Grandy laboratory at Oregon Health & Science University (OHSU), studying the underlying chemical biology of methamphetamine (Meth) addiction, this dissertation reports on the development of six new thyronamine ...
Wahl, Troy Andrew
core   +1 more source

Novel 1-Amidino-4-Phenylpiperazines as Potent Agonists at Human TAAR1 Receptor: Rational Design, Synthesis, Biological Evaluation and Molecular Docking Studies

Pharmaceuticals, 2020
Targeting trace amine-associated receptor 1 (TAAR1) receptor continues to offer an intriguing opportunity to develop innovative therapies in different pharmacological settings.
Valeria Francesconi, Elena Cichero, Evgeny V. Kanov, Erik Laurini, Sabrina Pricl, Raul R. Gainetdinov, Michele Tonelli   +6 more
doaj   +1 more source

Sensory Gating in TAAR1 Knockout Mice

Journal of Evolutionary Biochemistry and Physiology, 2022
Abstract Trace amines (TA) are a family of endogenous compounds structurally similar to classical biogenic amines that may be involved in the pathogenesis of a number of neuropsychiatric disorders. One of the most studied and perspective member of the TA associated receptors (TAARs) family is the TAAR1.
A. A. Aleksandrov, E. S. Dmitrieva, V. M. Knyazeva, Y. A. Simon, N. V. Polyakova, L. N. Stankevich, A. Y. Aleksandrov   +6 more
openaire   +1 more source